midterm drugs, NT's, and receptors Flashcards
Pargyline
MAO inhibitor
Cocaine
NE reuptake inhibitor
potentiates sympathetic respone
Imipramine
NE reuptake inhibitor
tricyclic antidepressant
potentiates sympathetic respone
Tyramine
reverses axoplasmic pumps
more NE in synapse
amphetamine
reverses axoplasmic pumps
more NE in synapse
ephedrine
reverses axoplasmic pumps
more NE in synapse
Reserpine
blocks vesicular accumulation of NE
decreases available NE
guanethidine/guanadrel
releases NE from vesicles
depletes NE
epinephrine MOA (receptors):
agonist of a1, a2, B1, B2
B > a, but alpha effects predominate at high doses
Isoproterenol
activates B1, B2
Phenylephrine
activates a1
Dobutamine
activates B1
Albuterol
activates B2
bronchial SM relaxation (acute exacerbation)
metaproterenol
activates B2
bronchial SM relaxation
ritodrine
B2 agonist
delays labor
terbutaline
B2 agonist
delay labor
salmeterol
B2 agonist
long acting asthma prophylaxis
B2 receptors have higher affinity for Epi or NE?
Epi
B1 is about equal
Binds to penicillin binding proteins and inhibits peptidoglycan synthesis. Broad spectrum for Gram negative organisms.
Ceftriaxone
Forms H-bonds with D-ala-D-alanine and prevents the incorporation of NAM/NAG-peptide subunits into peptidoglycan matrix. Broad spectrum for Gram positive organisms.
Vancomycin
Beta- lactam ring binds to DD-transpeptidase inhibiting cross-linking for remodeling of peptidoglycan. Inhibits transpeptidase. Narrow spectrum of Gram positive, aerobic organisms.
Penicillin G
Converts plasminogen to plasmin –> degrades clots
tPA (alteplase)
Inhibits COX1/TXA2 –> inhibiting platelet aggregation
aspirin
Binds to opioid receptors in the CNS, causing inhibition of ascending pain pathways, altering the perception of and response to pain; produces generalized CNS depression.
morphine
forms free radical nitric oxide. In smooth muscle, activates guanylate cyclase which increases guanosine 3’5’ monophosphate (cGMP) leading to dephosphorylation of myosin light chains and smooth muscle relaxation.
vasodilator effect on the peripheral veins and arteries with more prominent effects*** on the veins.
NTG
competitive inhibitor of glycoprotein (GP) IIb/IIIa preventing the binding of fibrinogen, von Willebrand factor (vWF), and other adhesive ligands to the GP IIb/IIIa receptor on activated platelets.
***works when ASA will not
Eptifibatide
inhibition of histamine at H2-receptors of the gastric parietal cells
ranitidine
Blocks ADP receptors on platelets → inhibits platelet activation
clopidogrel
↑ Activity of antithrombin III → inhibits thrombin (and others in coagulation cascade)→ blocks conversion of fibrinogen → fibrin = no clot ☺
heparin
Inhibit cholesterol synthesis.
HMG-CoA reductase inhibitors.
statins
Suppresses RAAS system by inhibiting conversion of Angiotensin I to Angiotensin II. Net effects:
• Decreased Aldosterone release → Decreased Na reabsorption in kidney → decreased blood volume and preload
ACE inhibitors
names end in “pril”
specifically blocks Beta1 receptors
• Main activity on heart → decrease heart rate and contractility thus decreasing myocardial oxygen demand
• Decreases BP
metoprolol
***not in acute CHF….need to get fluid off first
non-specific (blocks Beta 1 and 2)
propanolol
Same mechanism as nitroglycerine
***longer half life
isosorbide dinitrate
Increases NO synthesis in endothelium.
Higher selectivity for arterioles–> decreased afterload
hydralazine
Inhibits NKCC2 (the luminal symporter in thick ascending limb of loop of Henle) → ↓ reabsorption of Na+ and Cl- → Increased Na+ & water excretion → ↓Blood Volume →↓Preload
furosemide
Blocks aldosterone action. Net effects:
• Decreases Na reabsorption in kidney → decreases blood volume and preload
spironolactone
eplerenone
Inhibits Na/K ATPase:
• Increased Na intracellular concentration
• Increased Na/Ca co-transporter activity
• Increased intracellular Ca++
• INCREASED CONTRACTILIY (positive ionotrope)
ALSO – prolongs nodal action potentials thus DECREASING HEART RATE
digoxin
***high toxicity–used in refractory acute CHF
AMINO-Beta-Lactam: Binds P.B.P. and blocks transpeptidation of peptidoglycan in bacterial cell walls.
amoxixillin
beta-lactamase inhibitor
clavulanate
add to amoxiccilin
contraindication for tPA?
endocarditis
purpose of B-blockers in MI tx?
reduce ischemia (decreases myocardial oxygen demand)